General Information of Drug Therapeutic Target (DTT) (ID: TT1MPAY)

DTT Name GABA(A) receptor alpha-1 (GABRA1)
Synonyms Gamma-aminobutyric acid receptor subunit alpha-1; GABA(A) receptor subunit alpha-1
Gene Name GABRA1
DTT Type
Successful target
[1]
Related Disease
Acute respiratory distress syndrome [ICD-11: CB00]
Anxiety disorder [ICD-11: 6B00-6B0Z]
Chronic insomnia [ICD-11: 7A00]
Chronic pain [ICD-11: MG30]
Corneal disease [ICD-11: 9A76-9A78]
Cystitis [ICD-11: GC00]
Depression [ICD-11: 6A70-6A7Z]
Epilepsy/seizure [ICD-11: 8A61-8A6Z]
Headache [ICD-11: 8A80-8A84]
Insomnia [ICD-11: 7A00-7A0Z]
Malaria [ICD-11: 1F40-1F45]
Mental/behavioural/neurodevelopmental disorder [ICD-11: 6E20-6E8Z]
Tonus and reflex abnormality [ICD-11: MB47]
BioChemical Class
Ligand-gated ion channel
UniProt ID
GBRA1_HUMAN
TTD ID
T51487
3D Structure
Download
2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MRKSPGLSDCLWAWILLLSTLTGRSYGQPSLQDELKDNTTVFTRILDRLLDGYDNRLRPG
LGERVTEVKTDIFVTSFGPVSDHDMEYTIDVFFRQSWKDERLKFKGPMTVLRLNNLMASK
IWTPDTFFHNGKKSVAHNMTMPNKLLRITEDGTLLYTMRLTVRAECPMHLEDFPMDAHAC
PLKFGSYAYTRAEVVYEWTREPARSVVVAEDGSRLNQYDLLGQTVDSGIVQSSTGEYVVM
TTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISA
RNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRGYAWDGKSVVPEKPKKVKDP
LIKKNNTYAPTATSYTPNLARGDPGLATIAKSATIEPKEVKPETKPPEPKKTFNSVSKID
RLSRIAFPLLFGIFNLVYWATYLNREPQLKAPTPHQ
Function
Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain. Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel. The gamma2 subunit is necessary but not sufficient for a rapid formation of active synaptic contacts and the synaptogenic effect of this subunit is influenced by the type of alpha and beta subunits present in the receptor pentamer (By similarity). The alpha1/beta2/gamma2 receptor and the alpha1/beta3/gamma2 receptor exhibit synaptogenic activity. GABRA1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Functions also as histamine receptor and mediates cellular responses to histamine (By similarity).
KEGG Pathway
Neuroactive ligand-receptor interaction (hsa04080 )
Retrograde endocannabinoid signaling (hsa04723 )
GABAergic synapse (hsa04727 )
Morphine addiction (hsa05032 )
Nicotine addiction (hsa05033 )
Reactome Pathway
GABA A receptor activation (R-HSA-977441 )
Ligand-gated ion channel transport (R-HSA-975298 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
25 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Allopregnanolone DMNLHAC Depression 6A70-6A7Z Approved [2]
Amobarbital DM0GQ8N Insomnia 7A00-7A0Z Approved [1], [3]
Barbital DMJ8NMC Insomnia 7A00-7A0Z Approved [1], [3]
Barbiturate DMJIA6T Anaesthesia 9A78.6 Approved [1], [3]
Butabarbital DMC5AST Insomnia 7A00-7A0Z Approved [1], [4], [3]
Butalbital DM9J04X Anxiety disorder 6B00-6B0Z Approved [1]
Butethal DM7JHX0 Insomnia 7A00-7A0Z Approved [1]
Clobazam - Lundbeck DMW1OQ0 Anxiety disorder 6B00-6B0Z Approved [1]
Ethanol DMDRQZU Chronic pain MG30 Approved [1]
Ethchlorvynol DM53IP1 Insomnia 7A00-7A0Z Approved [1]
Hexobarbital DMQ314B Anaesthesia 9A78.6 Approved [1], [3]
Indiplon DMOPGHQ Fibromyalgia MG30.01 Approved [5], [6]
Meprobamate DMHM93Y Anxiety disorder 6B00-6B0Z Approved [1]
Methohexital DM7YMIT Anaesthesia 9A78.6 Approved [1]
Methoxyflurane DML0RAE Anaesthesia 9A78.6 Approved [1]
Methylphenobarbital DMDSWAG Anxiety disorder 6B00-6B0Z Approved [1], [3]
Methyprylon DMBW7VH Insomnia 7A00-7A0Z Approved [1]
Nitrazepam DMEGIQ6 Epilepsy 8A60-8A68 Approved [1]
Pentobarbital DMFNH7L Insomnia 7A00-7A0Z Approved [1], [3]
Picrotoxin DMIBNG2 Respiratory distress syndrome CB00 Approved [1]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [1]
Secobarbital DM14RF5 Intractable insomnia 7A00 Approved [1], [3]
THIOCOLCHICOSIDE DMEPWYA Muscle spasm MB47.3 Approved [7]
Zaleplon DMGFWSM Insomnia 7A00-7A0Z Approved [8]
Zolpidem DMWOSKJ Insomnia 7A00-7A0Z Approved [9]
------------------------------------------------------------------------------------
⏷ Show the Full List of 25 Approved Drug(s)
3 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ZK-93423 DMFWMKZ Epileptic seizures 8A61-8A6Z Phase 3 [10]
EVT-201 DMQGBM1 Insomnia 7A00-7A0Z Phase 2 [11]
GSK683699 DMTW79H Inflammatory bowel disease DD72 Phase 2 [7]
------------------------------------------------------------------------------------
4 Discontinued Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
ELTANOLONE DM38CIV Premenstrual syndrome GA34.40 Discontinued in Phase 3 [2]
U-78875 DM2WOPX Anxiety disorder 6B00-6B0Z Discontinued in Phase 1 [12]
CGS-9896 DM39PQI N. A. N. A. Terminated [13]
Divaplon DMO3XBP N. A. N. A. Terminated [14]
------------------------------------------------------------------------------------
161 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
(2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid DMLEZKJ Discovery agent N.A. Investigative [15]
(2E,4S)-4-ammoniopent-2-enoate DMA9RIS Discovery agent N.A. Investigative [16]
(4R)-4-ammoniopentanoate DMZFTI4 Discovery agent N.A. Investigative [16]
(4S)-4-ammoniopentanoate DMBLAY1 Discovery agent N.A. Investigative [16]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol DMAXS9H Discovery agent N.A. Investigative [17]
(9-Benzyl-9H-purin-6-yl)-cyclopropyl-amine DMHJG5N Discovery agent N.A. Investigative [18]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester DMKI2Y9 Discovery agent N.A. Investigative [19]
(9H-beta-Carbolin-3-yl)-ethyl-amine DMVHMPC Discovery agent N.A. Investigative [19]
(9H-beta-Carbolin-3-yl)-methanol DMUF16A Discovery agent N.A. Investigative [17]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid DMVWQ26 Discovery agent N.A. Investigative [20]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one DMOGHRS Discovery agent N.A. Investigative [21]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one DM1KND6 Discovery agent N.A. Investigative [22]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole DMVCHSI Discovery agent N.A. Investigative [13]
1-(9H-beta-Carbolin-3-yl)-butan-1-one DMA96U5 Discovery agent N.A. Investigative [23]
1-(9H-beta-Carbolin-3-yl)-ethanone DMFOD2L Discovery agent N.A. Investigative [17]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one DMX2FWN Discovery agent N.A. Investigative [21]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide DMFAME4 Discovery agent N.A. Investigative [20]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one DM9RAYC Discovery agent N.A. Investigative [24]
2-(3-Bromo-phenyl)-chromen-4-one DM7XDLO Discovery agent N.A. Investigative [24]
2-(3-Chloro-phenyl)-chromen-4-one DML83DM Discovery agent N.A. Investigative [24]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline DMSB0JA Discovery agent N.A. Investigative [25]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one DMYGRS9 Discovery agent N.A. Investigative [13]
2-(9-Benzyl-9H-purin-6-ylamino)-ethanol DMPJ0O6 Discovery agent N.A. Investigative [18]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one DMHT80R Discovery agent N.A. Investigative [26]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline DM1F4TN Discovery agent N.A. Investigative [25]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline DMD2ZNA Discovery agent N.A. Investigative [25]
2-Oxa-spiro[4.4]nonan-1-one DM2NEX4 Discovery agent N.A. Investigative [21]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one DMJIVL3 Discovery agent N.A. Investigative [26]
2-Phenyl-3H-imidazo[4,5-c]quinoline DML9DJP Discovery agent N.A. Investigative [25]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline DMUIYZB Discovery agent N.A. Investigative [26]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one DMA1RHE Discovery agent N.A. Investigative [26]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one DMLCDZN Discovery agent N.A. Investigative [26]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline DMPF598 Discovery agent N.A. Investigative [25]
3,3-Diethyl-dihydro-furan-2-one DMFJ9N0 Discovery agent N.A. Investigative [21]
3,3-Diisopropyl-dihydro-furan-2-one DMIFUDG Discovery agent N.A. Investigative [21]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline DMSCIP2 Discovery agent N.A. Investigative [23]
3-(3-Methyl-butoxy)-9H-beta-carboline DMTNCXP Discovery agent N.A. Investigative [23], [27]
3-(benzyloxy)-9H-pyrido[3,4-b]indole DMDNEKR Discovery agent N.A. Investigative [27]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole DMKHNTY Discovery agent N.A. Investigative [27]
3-amino-3-demethoxythiocolchicine DM60K7H Discovery agent N.A. Investigative [7]
3-Butoxy-9H-beta-carboline DMQ8H74 Discovery agent N.A. Investigative [23], [27]
3-butoxycarbonyl-4-quinolone DMRF2Q8 Discovery agent N.A. Investigative [28]
3-butoxycarbonyl-6-ethyl-4-quinolone DMD6PMZ Discovery agent N.A. Investigative [28]
3-butylaminocarbonyl-6-ethyl-4-quinolone DM95XWR Discovery agent N.A. Investigative [28]
3-carboxy-6-ethyl-4-quinolone DMRUX93 Discovery agent N.A. Investigative [28]
3-Chloro-9H-beta-carboline DMCD901 Discovery agent N.A. Investigative [29]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone DMEL8S5 Discovery agent N.A. Investigative [28]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine DME8VPC Discovery agent N.A. Investigative [7]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine DMALMGH Discovery agent N.A. Investigative [7]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine DMXFVD1 Discovery agent N.A. Investigative [7]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine DM4ERYF Discovery agent N.A. Investigative [7]
3-demethoxy-3D-glucopyranosylaminothiocolchicine DMID7TC Discovery agent N.A. Investigative [7]
3-Ethoxy-9H-beta-carboline DM6K7BI Discovery agent N.A. Investigative [29], [27]
3-ethoxycarbonyl-4-quinolone DMY4VOI Discovery agent N.A. Investigative [28]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone DMMDOI4 Discovery agent N.A. Investigative [28]
3-ethoxycarbonyl-6-propyl-4-quinolone DM1E5QZ Discovery agent N.A. Investigative [28]
3-Ethyl-3-isopropyl-dihydro-furan-2-one DMZK13I Discovery agent N.A. Investigative [21]
3-Ethyl-3-methyl-dihydro-furan-2-one DM1VTFU Discovery agent N.A. Investigative [21]
3-Isobutoxy-9H-beta-carboline DM6X5TZ Discovery agent N.A. Investigative [23], [27]
3-Isopropoxy-9H-beta-carboline DM7PHO4 Discovery agent N.A. Investigative [23]
3-Isopropyl-3-methyl-dihydro-furan-2-one DMSLPGZ Discovery agent N.A. Investigative [21]
3-Isothiocyanato-9H-beta-carboline DM9LEWH Discovery agent N.A. Investigative [30]
3-Methoxy-9H-beta-carboline DMTBX0D Discovery agent N.A. Investigative [29]
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium DMQMT1A Discovery agent N.A. Investigative [31]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one DMTM6B0 Discovery agent N.A. Investigative [22]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one DM870UV Discovery agent N.A. Investigative [22]
3-Methyl-9H-beta-carboline DMEJKZN Discovery agent N.A. Investigative [32]
3-Nitro-9H-beta-carboline DM08V9W Discovery agent N.A. Investigative [29]
3-Propoxy-9H-beta-carboline DMDEV64 Discovery agent N.A. Investigative [29], [27]
3-sec-Butoxy-9H-beta-carboline DMNP8DQ Discovery agent N.A. Investigative [23]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one DMGDT8V Discovery agent N.A. Investigative [21]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol DMCS538 Discovery agent N.A. Investigative [33]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole DMJI6QH Discovery agent N.A. Investigative [13]
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol DM1T95Y Discovery agent N.A. Investigative [34]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol DMZ18OJ Discovery agent N.A. Investigative [35]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol DMA4CZK Discovery agent N.A. Investigative [36]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline DMCS83F Discovery agent N.A. Investigative [37]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol DMV19HC Discovery agent N.A. Investigative [35]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol DMEIA3L Discovery agent N.A. Investigative [36]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol DM9O8UM Discovery agent N.A. Investigative [36]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol DM7E4JU Discovery agent N.A. Investigative [36]
5-(4-piperidyl)-4-propylisothiazol-3-ol DMZ7K5G Discovery agent N.A. Investigative [35]
5-(piperidin-4-yl)isothiazol-3-ol DM4XGFW Discovery agent N.A. Investigative [35]
5-(piperidin-4-yl)isoxazol-3-ol DM6GO2I Discovery agent N.A. Investigative [36]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate DM23PL4 Discovery agent N.A. Investigative [16]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate DMYAPLT Discovery agent N.A. Investigative [16]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one DMOIFAP Discovery agent N.A. Investigative [21]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one DM7FMWS Discovery agent N.A. Investigative [21]
6-benzyl-3-ethoxycarbonyl-4-quinolone DMICRFQ Discovery agent N.A. Investigative [28]
6-benzyl-3-propoxycarbonyl-4-quinolone DMXMI5E Discovery agent N.A. Investigative [28]
6-benzyl-3-propylaminocarbonyl-4-quinolone DM7HNPJ Discovery agent N.A. Investigative [28]
6-Bromo-2-(2-nitro-phenyl)-chromen-4-one DM7U58O Discovery agent N.A. Investigative [38]
6-Bromo-2-(3-bromo-phenyl)-chromen-4-one DMTJRF3 Discovery agent N.A. Investigative [24]
6-Bromo-2-(3-nitro-phenyl)-chromen-4-one DMP8ZVS Discovery agent N.A. Investigative [38]
6-Bromo-2-(4-nitro-phenyl)-chromen-4-one DMCX3TM Discovery agent N.A. Investigative [38]
6-Bromo-2-phenyl-chromen-4-one DMMCNQI Discovery agent N.A. Investigative [24]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone DM4HRIX Discovery agent N.A. Investigative [28]
6-bromo-3-ethoxycarbonyl-4-quinolone DM0MQHP Discovery agent N.A. Investigative [28]
6-Chloro-2-(3-nitro-phenyl)-chromen-4-one DMTWBOV Discovery agent N.A. Investigative [24]
6-Chloro-2-phenyl-chromen-4-one DM5FZDI Discovery agent N.A. Investigative [24]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone DMLEUP2 Discovery agent N.A. Investigative [28]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone DMESU53 Discovery agent N.A. Investigative [28]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone DM1POEA Discovery agent N.A. Investigative [28]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone DMG05V1 Discovery agent N.A. Investigative [28]
6-ethyl-3-i-propoxycarbonyl-4-quinolone DML9EU7 Discovery agent N.A. Investigative [28]
6-ethyl-3-pentoxycarbonyl-4-quinolone DMSGJM6 Discovery agent N.A. Investigative [28]
6-ethyl-3-propoxycarbonyl-4-quinolone DMGVI08 Discovery agent N.A. Investigative [28]
6-ethyl-3-propylaminocarbonyl-4-quinolone DMC1F2E Discovery agent N.A. Investigative [28]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one DMPZIV0 Discovery agent N.A. Investigative [24]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one DMNJRFP Discovery agent N.A. Investigative [21]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one DMRCTBA Discovery agent N.A. Investigative [39]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one DMM635K Discovery agent N.A. Investigative [39]
6-Nitro-2-phenyl-chromen-4-one DMVLID9 Discovery agent N.A. Investigative [24]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene DM3FXRC Discovery agent N.A. Investigative [40]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene DMTZ943 Discovery agent N.A. Investigative [29]
9H-beta-Carbolin-3-ol DMBWAMR Discovery agent N.A. Investigative [29]
9H-beta-Carbolin-6-ylamine DMBLEI7 Discovery agent N.A. Investigative [17]
9H-beta-Carboline-3-carboxylic acid ethyl ester DMK459I Discovery agent N.A. Investigative [27], [41]
9H-beta-Carboline-3-carboxylic acid propyl ester DMMUH98 Discovery agent N.A. Investigative [41]
AMENTOFLAVONE DMLRNV2 Discovery agent N.A. Investigative [42]
Barbituric acid derivative DM2I19P Discovery agent N.A. Investigative [43]
Benzyl-(9H-beta-carbolin-6-yl)-amine DMW167A Discovery agent N.A. Investigative [29]
Beta-Carboline-3-carboxylic acid t-butyl ester DM9LT60 N. A. N. A. Investigative [27]
BETA-CCM DM1MFTZ Discovery agent N.A. Investigative [44]
CGS-13767 DM4DSE7 Discovery agent N.A. Investigative [45]
CGS-9895 DMKY6CU Discovery agent N.A. Investigative [46]
CI-218872 DM0RH3S Discovery agent N.A. Investigative [32]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate DM5G91Z Discovery agent N.A. Investigative [27]
Flavone DMEQH6J Discovery agent N.A. Investigative [24]
GNF-PF-3645 DM17GIV Discovery agent N.A. Investigative [28]
GNF-PF-4421 DMV10UH Discovery agent N.A. Investigative [28]
Isoquinoline-3-carboxylic acid methyl ester DMWIMUZ Discovery agent N.A. Investigative [29]
L-655708 DM4CDIB Discovery agent N.A. Investigative [47]
N-(9H-beta-Carbolin-3-yl)-acetamide DMBD52I Discovery agent N.A. Investigative [19]
N-(9H-beta-Carbolin-3-yl)-formamide DM3KNSY Discovery agent N.A. Investigative [19]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide DMULBO9 Discovery agent N.A. Investigative [48]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide DM8A23B Discovery agent N.A. Investigative [48]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide DMMT65J Discovery agent N.A. Investigative [48]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide DM157LQ Discovery agent N.A. Investigative [48]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide DMH7Z4L Discovery agent N.A. Investigative [48]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide DM8ZMB5 Discovery agent N.A. Investigative [49]
NORHARMANE DMKYQWG Discovery agent N.A. Investigative [29]
NSC-73613 DMT6CV5 Discovery agent N.A. Investigative [24]
NSC-93394 DM2JPD4 Discovery agent N.A. Investigative [24]
Pyrrolidin-3-yl-acetic acid DM0BHCJ Discovery agent N.A. Investigative [50]
Ridine-5-carboxylic acid ethyl ester DM9HMCS Discovery agent N.A. Investigative [51]
RIPAZEPAM DMTHVQD Discovery agent N.A. Investigative [52]
RO-054520 DM78B4A Discovery agent N.A. Investigative [53]
RO-145974 DM0ACKJ Discovery agent N.A. Investigative [54]
RO-145975 DMAJ6BW Discovery agent N.A. Investigative [54]
RO-147437 DMX4B36 Discovery agent N.A. Investigative [54]
Ro-15-3505 DM4NW3U Discovery agent N.A. Investigative [54]
RO-194603 DM8C2Z0 Discovery agent N.A. Investigative [54]
Ro-4938581 DMCB2N9 Discovery agent N.A. Investigative [55]
RWJ-16979 DME68VT Discovery agent N.A. Investigative [56]
RY-066 DMGUX16 Discovery agent N.A. Investigative [57]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate DM9QSDC Discovery agent N.A. Investigative [27]
U-89267 DMQT6AH Discovery agent N.A. Investigative [58]
[3H]CGP27492 DMQTBRM Discovery agent N.A. Investigative [59]
[3H]CGS8216 DMLP68J Inflammation 1A00-CA43.1 Investigative [45]
[3H]Ro154513 DMMBWKL Discovery agent N.A. Investigative [54]
------------------------------------------------------------------------------------
⏷ Show the Full List of 161 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Major depressive disorder 6A20 Pre-frontal cortex 9.57E-01 -0.12 -0.18
------------------------------------------------------------------------------------

References

1 DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6.
2 Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9.
3 Effect of barbiturates on polyphosphoinositide biosynthesis and protein kinase C activity in synaptosomes. Neuropharmacology. 1989 Dec;28(12):1317-23.
4 Hypnotic drugs. Med Lett Drugs Ther. 2000 Aug 7;42(1084):71-2.
5 Emerging therapies for fibromyalgia. Expert Opin Emerg Drugs. 2008 Mar;13(1):53-62.
6 Glutamate- and GABA-based CNS therapeutics. Curr Opin Pharmacol. 2006 Feb;6(1):7-17.
7 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
8 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
9 Zolpidem, a selective GABA(A) receptor alpha1 subunit agonist, induces comparable Fos expression in oxytocinergic neurons of the hypothalamic paraventricular and accessory but not supraoptic nuclei in the rat.Brain Res Bull.2006 Dec 11;71(1-3):200-7.
10 Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9.
11 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
12 Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. J Med Chem. 1999 Apr 8;42(7):1123-44.
13 Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. J Med Chem. 2006 Mar 23;49(6):1855-66.
14 (Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics. J Med Chem. 1988 Jun;31(6):1220-6.
15 ( )-2-amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist. Bioorg. Med. Chem. Lett. 1(5):247-248 (1991).
16 gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
17 Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists. J Med Chem. 1987 Apr;30(4):750-3.
18 Benzodiazepine receptor binding activity of 6,9-disubstituted purines. J Med Chem. 1989 May;32(5):1020-4.
19 3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam. J Med Chem. 1985 Jun;28(6):824-8.
20 Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. J Med Chem. 1992 Jun 12;35(12):2214-20.
21 Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant ... J Med Chem. 1994 Jan 21;37(2):275-86.
22 Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ... J Med Chem. 1988 Jan;31(1):1-3.
23 Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach. J Med Chem. 1992 Oct 30;35(22):4001-10.
24 Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor, Bioorg. Med. Chem. Lett. 7(15):2003-2008 (1997).
25 Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51.
26 Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. J Med Chem. 1996 Jul 19;39(15):2915-21.
27 Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64.
28 4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore mod... J Med Chem. 2006 Apr 20;49(8):2526-33.
29 Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. J Med Chem. 1988 Sep;31(9):1854-61.
30 Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site. J Med Chem. 1990 Sep;33(9):2343-57.
31 N-2 methylated quaternary derivatives of beta-carboline-3-carboxylates inhibit acetylcholinesterase in vitroO, Bioorg. Med. Chem. Lett. 3(12):2831-2836 (1993).
32 Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem. 1994 Dec 23;37(26):4576-80.
33 Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of ga... J Med Chem. 2006 Jul 13;49(14):4442-6.
34 Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relatio... J Med Chem. 2010 Apr 22;53(8):3417-21.
35 Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. J Med Chem. 2006 Feb 23;49(4):1388-96.
36 Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. J Med Chem. 2005 Jan 27;48(2):427-39.
37 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
38 6-Bromo-3 nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites, Bioorg. Med. Chem. Lett. 7(3):373-378 (1997).
39 6,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties, Bioorg. Med. Chem. Lett. 5(22):2717-2720 (1995).
40 Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands. J Med Chem. 1987 Mar;30(3):456-8.
41 beta-Carbolines as benzodiazepine receptor ligands. 1. Synthesis and benzodiazepine receptor interaction of esters of beta-carboline-3-carboxylic a... J Med Chem. 1983 Apr;26(4):499-503.
42 Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
43 Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57.
44 Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high af... J Med Chem. 1995 Jan 6;38(1):189-98.
45 Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. J Med Chem. 1991 Jan;34(1):281-90.
46 1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. J Med Chem. 1987 Oct;30(10):1737-42.
47 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor li... J Med Chem. 2004 Mar 25;47(7):1807-22.
48 Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-... J Med Chem. 2007 Apr 5;50(7):1627-34.
49 Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular mo... J Med Chem. 2001 Jul 5;44(14):2286-97.
50 Orally active and potent inhibitors of gamma-aminobutyric acid uptake. J Med Chem. 1985 May;28(5):653-60.
51 Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. J Med Chem. 1989 Dec;32(12):2561-73.
52 Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in r... J Med Chem. 1985 May;28(5):683-5.
53 Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem. 1988 Dec;31(12):2235-46.
54 Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepin... J Med Chem. 1993 Apr 16;36(8):1001-6.
55 The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment... Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4.
56 Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. J Med Chem. 1995 Jan 6;38(1):16-20.
57 Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42.
58 Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. J Med Chem. 1994 Mar 18;37(6):758-68.
59 Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.